171670-07-8Relevant articles and documents
Enhancing Aromatic Foldamer Helix Dynamics to Probe Interactions with Protein Surfaces
Vallade, Ma?lle,Sai Reddy, Post,Fischer, Lucile,Huc, Ivan
, p. 5489 - 5498 (2018)
Dynamic helices that undergo exchange between P and M conformations can be used as sensors when their interactions with chiral substances results in a helix handedness bias. For instance, chiral induction in short helically folded aromatic oligoamides based on 8-amino-2-quinoline carboxylic acid (Q) has been used to detect interactions with proteins and nucleic acids. However, the stability of these helices in water increases rapidly with oligomer length to the extent that helix dynamics become too slow for sensing applications. We have developed an approach to enhance the helix dynamics of these oligomers through the introduction of more flexible 6-aminomethyl-2-pyridinecarboxylic acid units (P) while preserving helix integrity. A series of P/Q hybrid oligoamides were synthesized and their rate of helix handedness inversion was evaluated by monitoring induced circular dichroism so as to define the requirements to bring kinetics in a practical range for sequences as long as fourteen units. Proof of principle was then brought by confining such sequences at the surface of carbonic anhydrase and showing that protein-mediated helix handedness induction occurs.
Polysubstituted pyridine medical intermediate and synthetic method thereof
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Paragraph 0047; 0058, (2016/10/08)
The invention belongs to the field of medicine intermediate technology, and specifically relates to a polysubstituted pyridine medical intermediate and a synthetic method thereof. The polysubstituted pyridine medical intermediate is a key intermediate in pharmaceutical synthesis, and has a huge market potential. The synthetic method has simple synthetic route, simple and easily available staring material, and has great meaning in synthesis of pyridine intermediate, development of pyridine medicament and research and development of novel medicament, and the product is cheap.
CYCLIC PEPTIDE COMPOUND, AND PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE THEREOF
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Page/Page column 41, (2016/08/23)
The present invention relates to a cyclic peptide compound, and a preparation method, pharmaceutical composition and use thereof. In particular, the cyclic peptide compound of the present invention has a structure as shown by general formula (I). The compound of general formula (I), and isomers, racemates, pharmaceutically acceptable salts, crystalline hydrates, solvates or mixtures thereof have a use in the preparation of medicaments for preventing or treating mammalian diseases associated with histone deacetylase dysregulations.
Dimeric self-assembly of pyridyl guanidinium carboxylates in polar solvents
Irfan Ashiq, Muhammad,Tesfatsion, Biniam F.,Gaggini, Francesca,Dixon, Sally,Kilburn, Jeremy D.
experimental part, p. 12387 - 12397 (2011/02/22)
A series of pyridyl guanidinium-carboxylates has been prepared and the dimeric self-assembly of these studied in H2O/DMSO mixtures, principally using dilution isothermal calorimetry. Compounds 5 and 6, incorporating an aromatic ring in the "tet
4,6-DISUBSTITUTED PYRIMIDINES AND THEIR USE AS PROTEIN KINASE INHIBITORS
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Page/Page column 56, (2008/06/13)
The invention relates to novel pyrimidine derivatives of Formula (I), which are efficacious inhibitors of protein kinases, in particular of one or more isoforms of the protein kinase B/Akt.
